Several skin disorders are manifestations of an overreaction of the skin to androgenic stimulation. These include acne vulgaris, seborrhea, hirsutism (undesirable hairiness in women) and male-pattern baldness. Acne vulgaris is especially common among young adults. It is characterized by open and closed comedones, inflammatory papules, pustules, cysts and nodules of the face, chest and back. The disease afflicts primarily the sebaceous gland, which is sensitive to androgenic stimulation, and overreaction of the gland to androgens is an important aspect of the multifactoral pathology of acne. The disease can leave damaging scars, both physically and psychologically.
It is a common clinical observation that acne lesions often flare up or exacerbate when the patient is in a stressful situation. This is the time when the secretion of adrenal cortex is increased in response to stress. The most abundant steroids secreted by the adrenal cortex are dehydroepiandrosterone (DHA) and its sulfate. Although DHA has only weak androgenic activity, studies by the inventor and other laboratories have shown that it is readily metabolized in the skin to form potent androgenic steroids--androstenedione, testosterone and dihydrotestosterone (DHT). These steroids, especially DHT, cause increased sebaceous activity and aggravate acne lesions. Theoretically, it is desirable to arrest the conversion of DHA into these potent androgens in cases of acne vulgaris. In a recent study a significant correlation has been found between the activity of .DELTA..sup.5 -3.beta.-hydroxysteroid dehydrogenase .DELTA..sup.4-5 -isomerase in human sebaceous glands and their secretory activities (Simpson et al, J. Invest. Dermatol. 81:139-144, 1983). This enzymic activity is involved in the first step in the conversion of DHA into more potent androgens.
Presently available remedies for the treatment of acne vulgaris in the acute phase include the following:
Topical antibiotics--erythomycin, clincamycin.
Topical keratolytics--benzoyl peroxide, retinoic acid, sulfur.
Oral antibiotics--tetracycline and derivatives, erythromycin.
Vitamin A and derivatives--Vit. A, 25,000-50,000 Units daily, 13-Cis retinoic acid (Accutane).
Existing remedies for acne all have drawbacks, however. For example, topical application of retinoic acid or benzoyl peroxide irritates the skin and causes the skin to peel. The use of such agents, although effective in treating acne lesions in the acute phase of the disease, causes redness, irritation and undesirable appearance of the skin. The use of antibiotics has the undesirable side effects of changing the microbial environment of the body. The internal use of Accutane alters blood lipids and causes liver toxicity.
Clearly, a substance or composition exhibiting antiandrogenicity and which avoided the problems and drawbacks of the prior art would be useful to those who suffer the conditions resulting from over androgenicity of the skin. Such a composition is the subject of the present invention.